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Terbinafine

Terbinafine hydrochloride, sold as Lamisil tablets in the U.S., is often prescribed for the treatment of onychomycosis of the toenail or fingernail due to dermatophytes (Tinea unguium). more...

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It is also sold as a 1% cream or powder for use on suface infections such as jock itch (Tinea cruris) or athlete's foot (Tinea pedis).

Nail fungus infections live deep under the nail in the nail bed. Surface treatments may not be able to reach it in sufficient amounts, so terbinafine hydrochloride is given orally in tablet form, which is absorbed through the bloodstream to reach the infection; this method can cause hepatotoxicity, or liver damage, as well as other serious side effects, so those taking Lamisil tablets often have blood screenings every month. Many health insurance companies consider these infections to be a cosmetic problem, and either do not cover the cost of the months-long course of Lamisil, which can run into the thousands of dollars, or recommend use of less expensive alternatives like fluconazole.

The tablets contain the synthetic allylamine antifungal compound terbinafine hydrochloride, which is a white fine crystalline powder that is freely soluble in methanol and methylene chloride, soluble in ethanol, and slightly soluble in water. Chemically, it is (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1- naphthalenemethanamine hydrochloride. The empirical formula C21H26CIN with a molecular weight of 327.90

  • Active Ingredients: Terbinafine hydrochloride (equivalent to 250 mg base)
  • Inactive Ingredients: Colloidal silicon dioxide, Hydroxypropyl methylcellulose USP, Sodium starch glycolate, Magnesium stearate, Microcrystalline cellulose.

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In vitro susceptibility testing of ciclopirox, terbinafine, ketoconazole and itraconazole against dermatophytes and nondermatophytes, and in vitro evaluation
From Journal of Drugs in Dermatology, 12/1/03

Gupta AK, Kohli Y. Br J Dermatol 2003 Aug; 149(2):296-305.

The authors set out to determine the in vitro susceptibility of fungal organisms to ciclopirox, terbinafine, ketoconazole, and itraconazole, and to evaluate the in vitro activity and mode of interaction of ciclopirox in combination with either terbinafine or itraconazole. 133 strains were evaluated, including dermatophytes, Candida spp., and nondermatophyte molds. Some of the test medications had either additive, synergistic, or indifferent effects, but there were no cases of antagonism. The testing indicates that ciclopirox may have a broad antimicrobial profile including dermatophytes, yeasts, and other nondermatophytes. Terbinafine is extremely potent against dermatophytes. In vitro evaluation of activity of eiclopirox and terbinafine suggests many instances of synergy or additivism; for ciclopirox and itraconazole there may be indifference, synergy, or additivism.

JDD ARTICLE EVALUATION

In-vitro studies are a good start for any study, but once you see these organisms in-vivo you confront many complicating factors, such as competing bacteria, fungi, and environments. It would have been a more clinically relevant study if cultures of suspected patients (in-vivo) were performed and double-blinded studies involving the above medications were done. Some additive or synergistic effects are seen which can permit a lower dose of each of the medications; again, further studies are requires to recommend any therapies.

COPYRIGHT 2003 Journal of Drugs in Dermatology
COPYRIGHT 2004 Gale Group

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